Pharmacokinetic Insights and Therapeutic Potential of Calcium Channel Blockers in Cardiovascular and Non-Cardiovascular Disorders

Calcium channel blockers (CCBs) regulate calcium ion transport across cell membranes and are central to the management of hypertension, angina, arrhythmias, and cerebrovascular disorders, with emerging roles in neurological and oncological diseases. Most CCBs undergo significant first-pass metabolism mediated by cytochrome P450, which affects their interindividual variability, dosage, and bioavailability. Recent research highlights the potential of T-type CCBs in cancer treatment and the use of nanocarriers to overcome their low bioavailability and rapid metabolism. Since the introduction of verapamil in the 1960s, newer drugs with improved selectivity and safety, such as cilnidipine and azelnidipine, have been developed. Despite their widespread use, challenges remain in maximizing long-term efficacy, minimizing side effects, and individualizing treatment. This review provides an updated overview of the pharmacokinetics, pharmacodynamics, and therapeutic applications of dihydropyridine and non-dihydropyridine CCBs, while identifying research gaps and future directions to enhance their clinical utility. By integrating established pharmacological knowledge with recent advances, this study underscores the continued relevance of CCBs in modern medicine.